REVERSOL
Clinical safety rating: caution
Comprehensive clinical and safety monograph for REVERSOL (REVERSOL).
Reversal agent for neuromuscular blockade; inhibits acetylcholinesterase, increasing acetylcholine concentration at nicotinic receptors to reverse nondepolarizing neuromuscular blocking agents.
| Metabolism | Primarily hepatic via glucuronidation; minimal CYP450 involvement. |
| Excretion | Primarily renal excretion of unchanged drug (60-70%). Fecal elimination accounts for 20-25% via biliary secretion. Minor metabolism (<10%) with metabolites also renally cleared. |
| Half-life | Terminal elimination half-life is 8-12 hours in healthy adults (mean 10 hours). In hepatic impairment, increases up to 18 hours; in severe renal impairment (CrCl <30 mL/min), half-life may extend to 24 hours. |
| Protein binding | Approximately 95% bound, primarily to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | 1.5-2.0 L/kg, indicating extensive distribution into tissues, including central nervous system. |
| Bioavailability | Oral: 70-85% due to moderate first-pass metabolism. Intramuscular: ~100%. |
| Onset of Action | Intravenous: within 2-5 minutes. Oral: 30-60 minutes. Intramuscular: 10-15 minutes. |
| Duration of Action | Intravenous: 4-6 hours; oral: 6-8 hours; intramuscular: 3-5 hours. Duration is dose-dependent and may be prolonged in hepatic impairment. |
0.25-0.5 mg/kg IV bolus over 10 seconds, repeated if necessary up to a maximum total dose of 2 mg/kg.
| Dosage form | INJECTABLE |
| Renal impairment | No dose adjustment required for GFR ≥10 mL/min; avoid use if GFR <10 mL/min or in patients on renal replacement therapy due to accumulation of cyclodextrin excipient. |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B or C: use with caution; dose reduction of 50% recommended due to prolonged neuromuscular blocking effect. |
| Pediatric use | Neonates and infants: 0.15-0.2 mg/kg IV. Children 2-12 years: 0.2-0.5 mg/kg IV. Repeat doses at 0.5-1.0 times initial dose; maximum total 2 mg/kg. |
| Geriatric use | Elderly patients (>65 years): consider dose reduction by 20-30% due to increased sensitivity and prolonged recovery; monitor neuromuscular function closely. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for REVERSOL (REVERSOL).
| Breastfeeding | Excretion into human milk unknown; M/P ratio not determined. Caution recommended due to potential adverse effects in nursing infants. |
| Teratogenic Risk | First trimester: insufficient data in humans; animal studies show dose-dependent skeletal anomalies. Second and third trimesters: possible fetal growth restriction (limited evidence). Avoid in pregnancy unless benefit outweighs risk. |
| Fetal Monitoring |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
Hypersensitivity to sugammadex or any component; severe renal impairment (eGFR <30 mL/min/1.73 m^2).
| Precautions | Monitor for bradycardia, bronchospasm, and seizures. Use with caution in patients with asthma, COPD, or bradyarrhythmias. Avoid in patients with known hypersensitivity to sugammadex. |
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| Monitor maternal blood pressure, liver function tests, and complete blood count periodically. Fetal ultrasound for growth and amniotic fluid volume if used beyond 20 weeks gestation. |
| Fertility Effects | Animal studies show impaired fertility at high doses; human data insufficient. Possible reversible effect on sperm motility in males. |